ABSTRACT
Background: Atorvastatin (ATV), a lipid lowering agent, has low solubility and poor dissolution affects its oral bioavailability. Nanoemulsion (NE) has been developed to improve the delivery of therapeutic agents. This study was aimed to assess the ability of the NE in enhancing ATV bioavailability and minimizing its side effects in hyperlipidemic rats.Methods: Thirty-five rats divided into seven groups were utilized in this study. Hyperlipidemia was induced by feeding rats high fat diet (HFD) for 3 months. The antihyperlipidemic activity of 10 and 20 mg/kg of ATV loaded in two different delivery systems; nanoemulsion (10% and 20% ATV-LNE) or in water (10% and 20% ATV-sol), were investigated. At the end of the experiment, body weight, serum and plasma biochemical parameters (lipid profile, glucose, insulin, liver and kidney functions, oxidative stress markers were assessed. Liver and kidney were histopathologically examined. The physical characteristics of NE were determined by the Zetasizer (the z-average diameter and zeta potential).Results: 20% ATV-LNE had the smallest nanoparticles (38.12±6.71nm) whereas it had the largest zeta negative potential of -26.8±4.16mV. The serum biochemical results and the histopathological examination revealed that treatment with 20% ATV-LNE improved the lipid profile by significantly increasing HDL and decreasing cholesterol and low-density lipoprotein. Both 10 and 20% ATV-LNE reduced serum glucose level compared to other used formulas.Conclusions: NE formulas have the potential to improve the bioavailability and efficacy of ATV and reduce its side effects.